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1.
Pest Manag Sci ; 79(5): 1702-1712, 2023 May.
Artigo em Inglês | MEDLINE | ID: mdl-36594581

RESUMO

BACKGROUND: The two-spotted spider mite (TSSM), Tetranychus urticae (Acari: Tetranychidae), is a cosmopolitan phytophagous pest in agriculture and horticulture. It has developed resistance to many acaricides by target-site mutations. Understanding the status and evolution of resistant mutations in the field is essential for resistance management. Here, we applied a high-throughput Kompetitive allele-specific polymerase chain reaction (KASP) method for detecting six mutations conferring resistance to four acaricides of the TSSM. We genotyped 3274 female adults of TSSM from 43 populations collected across China in 2017, 2020, and 2021. RESULTS: The KASP genotyping of 24 testing individuals showed 99% agreement with Sanger sequencing results. KASP assays showed that most populations had a high frequency of mutations conferring avermectin (G314D and G326E) and pyridaben (H92R) resistance. The frequency of mutation conferring bifenazate (A269V and G126S) and etoxazole (I1017F) resistance was relatively low. Multiple mutations were common in the TSSM, with 70.2% and 24.6% of individuals having 2-6 and 7-10 of 10 possible resistant alleles, respectively. No loci were linked in most populations among the six mutations, indicating the development of multiple resistance is mainly by independent selection. However, G314D and I1017F on the nuclear genome deviated from Hardy-Weinberg equilibrium in most populations, indicating significant selective pressure on TSSM populations by acaricides or fitness cost of the mutations in the absence of acaricide selection. CONCLUSION: Our study revealed that the high frequency of TSSMs evolved multiple resistant mutations in population and individual levels by independent selection across China, alarming for managing multiple-acaricides resistance. © 2023 Society of Chemical Industry.


Assuntos
Acaricidas , Tetranychidae , Animais , Feminino , Acaricidas/farmacologia , Tetranychidae/genética , Alelos , Mutação , China
2.
Mar Drugs ; 15(11)2017 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-29104274

RESUMO

A series of bromophenol hybrids with N-containing heterocyclic moieties were designed, and their anticancer activities against a panel of five human cancer cell lines (A549, Bel7402, HepG2, HCT116 and Caco2) using MTT assay in vitro were explored. Among them, thirteen compounds (17a, 17b, 18a, 19a, 19b, 20a, 20b, 21a, 21b, 22a, 22b, 23a, and 23b) exhibited significant inhibitory activity against the tested cancer cell lines. The structure-activity relationships (SARs) of bromophenol derivatives were discussed. The promising candidate compound 17a could induce cell cycle arrest at G0/G1 phase and induce apoptosis in A549 cells, as well as caused DNA fragmentations, morphological changes and ROS generation by the mechanism studies. Furthermore, compound 17a suppression of Bcl-2 levels (decrease in the expression of the anti-apoptotic proteins Bcl-2 and down-regulation in the expression levels of Bcl-2) in A549 cells were observed, along with activation caspase-3 and PARP, which indicated that compound 17a induced A549 cells apoptosis in vitro through the ROS-mediated apoptotic pathway. These results might be useful for bromophenol derivatives to be explored and developed as novel anticancer drugs.


Assuntos
Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Organismos Aquáticos , Fenóis/farmacologia , Animais , Antineoplásicos/química , Linhagem Celular Tumoral/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Fenóis/química , Transdução de Sinais/efeitos dos fármacos , Relação Estrutura-Atividade
3.
Mini Rev Med Chem ; 17(8): 683-692, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-26471967

RESUMO

BACKGROUND: The widespread application of fluorine in drug design benefits from distinctive properties. Incorporation of fluorine can positively modulate certain pharmacokinetics properties, including lipophilicity, eletrophilicity, metabolic stability, chemical stability, et al., which were of interest to medicinal chemists. Herein, fluorinated compounds, which have been designed and evaluated for anticancer, antimicrobial, anti-inflammatory and antivirus activity, et al. during the last 6 years (2010-2015) are summarized. CONCLUSION: The emphasis is to highlight the importance of fluorinated compounds and the changes in the properties of compounds when introducing fluorine atom.


Assuntos
Anti-Infecciosos/farmacologia , Anti-Inflamatórios não Esteroides/farmacologia , Antineoplásicos/farmacologia , Antivirais/farmacologia , Desenho de Fármacos , Flúor/farmacologia , Animais , Anti-Infecciosos/síntese química , Anti-Infecciosos/química , Anti-Inflamatórios não Esteroides/síntese química , Anti-Inflamatórios não Esteroides/química , Antineoplásicos/síntese química , Antineoplásicos/química , Antivirais/síntese química , Antivirais/química , Flúor/química , Humanos
4.
Mini Rev Med Chem ; 15(2): 104-22, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-25643610

RESUMO

Diabetes mellitus, including type 1 and type 2 diabetes mellitus (2-DM) are the main threats to human health in the worldwide. Protein tyrosine phosphatase 1B (PTP1B) is a promising molecular level legitimate therapeutic target in the effective management of 2-DM. For the search of potent PTP1B inhibitors, much investigation has revealed a large number of small-molecule compounds obtained from natural sources or prepared by synthesis/semi-synthesis with various skeletons and promising anti-PTP1B activities in the treatment of 2-DM. Although some reviews on the development of PTP1B inhibitors have been published, they were mainly concentrated on the results reported in journal articles. In this review, we will provide an overview of the developments of the potent PTP1B inhibitors claimed in recent patents during the past five years (2009-2013) with their structural features and biological features, as well as the structure-activity relationships (SARs) and strategies for finding potent and specific PTP1B inhibitors. This paper will provide valuable information for understanding the current anti-PTP1B investigation and developing potent PTP1B inhibitors as treating 2-DM drugs.


Assuntos
Diabetes Mellitus Tipo 2/tratamento farmacológico , Inibidores Enzimáticos/farmacologia , Proteína Tirosina Fosfatase não Receptora Tipo 1/antagonistas & inibidores , Diabetes Mellitus Tipo 2/enzimologia , Inibidores Enzimáticos/química , Humanos , Relação Estrutura-Atividade
5.
Mar Drugs ; 13(2): 806-23, 2015 Feb 02.
Artigo em Inglês | MEDLINE | ID: mdl-25648512

RESUMO

A series of bromophenol derivatives containing indolin-2-one moiety were designed and evaluated that for their anticancer activities against A549, Bel7402, HepG2, HeLa and HCT116 cancer cell lines using MTT assay in vitro. Among them, seven compounds (4g-4i, 5h, 6d, 7a, 7b) showed potent activity against the tested five human cancer cell lines. Wound-healing assay demonstrated that compound 4g can be used as a potent compound for inactivating invasion and metastasis by inhibiting the migration of cancer cells. The structure-activity relationships (SARs) of bromophenol derivatives had been discussed, which were useful for exploring and developing bromophenol derivatives as novel anticancer drugs.


Assuntos
Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Indóis/síntese química , Indóis/farmacologia , Fenóis/síntese química , Fenóis/farmacologia , Linhagem Celular Tumoral , Movimento Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Espectroscopia de Ressonância Magnética , Invasividade Neoplásica/prevenção & controle , Metástase Neoplásica/prevenção & controle , Relação Estrutura-Atividade , Cicatrização/efeitos dos fármacos
6.
Zootaxa ; 3884(4): 379-86, 2014 Nov 17.
Artigo em Inglês | MEDLINE | ID: mdl-25543795

RESUMO

One new species of the genus Apotrechus from China is described, i.e. Apotrechus trilobus Bian & Shi sp. nov.. Meanwhile, a key to the species and the morphological photographs for five Chinese known species are provided in this paper. All material is deposited in the Museum of Hebei University.


Assuntos
Ortópteros/anatomia & histologia , Ortópteros/classificação , Distribuição Animal , Animais , China , Feminino , Masculino , Ortópteros/fisiologia , Especificidade da Espécie
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